Department of Pharmacognosy and Phytochemistry, Meiji Pharmaceutical University, 2-522-1 Noshio, Kiyose-shi, Tokyo 204-8588, Japan.
Bioorg Med Chem Lett. 2012 Jul 15;22(14):4793-800. doi: 10.1016/j.bmcl.2012.05.058. Epub 2012 Jun 1.
The research in our laboratory focuses on the isolation of saponins from cactus. In this study, we report five new triterpenoid saponins, dumortierinoside A methyl ester (1), pachanoside I1 (2), pachanoside D1 (3), gummososide A (4), and gummososide A methyl ester (5). Compounds 1-3 isolated from Isolatocereus dumortieri Backbg., and compounds 4 and 5 were isolated from Stenocereus alamosensis A. C. Gibson & K. E. Horak. Compound 2 possessed a new pachanane-type triterpene skeleton, pachanol I, in its aglycon. The aglycon of 3 was pachanol D, while those of 4 and 5 were both gummosogenin, which we have previously reported, but this is the first report of pachanol D and gummosogenin in their aglycon forms. Additionally, we evaluated the anti-type I allergy activity of the saponins with RBL-2H3 (Rat basophilic leukemia) cells by measuring the β-hexosaminidase release inhibitory activity. As a result of these studies, gummososide A methyl ester (5) was found to show activity (IC(50)=99.5 μM) and thurberoside A exhibited mild activity (IC(50)=166.9 μM).
本实验室的研究重点是从仙人掌中分离皂角苷。在这项研究中，我们报告了五个新的三萜皂苷，分别是：毛喉鞘蕊花苷甲酯（1）、巴卡诺苷 I1（2）、巴卡诺苷 D1（3）、古莫索苷 A（4）和古莫索苷 A 甲酯（5）。化合物 1-3 从 Isolatocereus dumortieri Backbg. 中分离得到，化合物 4 和 5 从 Stenocereus alamosensis A. C. Gibson & K. E. Horak 中分离得到。化合物 2 的苷元为具有新型巴卡烷型三萜骨架的巴卡醇 I，化合物 3 的苷元为巴卡醇 D，而化合物 4 和 5 的苷元均为古莫索苷元，这是我们之前报道过的，但这是首次报道巴卡醇 D 和古莫索苷元以苷元形式存在。此外，我们还通过测量β-己糖胺酶释放抑制活性，评估了 RBL-2H3（大鼠嗜碱性白血病）细胞中皂苷的抗 I 型过敏活性。研究结果表明，古莫索苷 A 甲酯（5）具有活性（IC50=99.5 μM），而噻伯苷 A 表现出轻微的活性（IC50=166.9 μM）。
